T-226296
T-226296 is an oral active and selective melanin-concentrating hormone receptor antagonist with the IC50 values of 5.5 nM and 8.6 nM for human SLC-1 and rat SLC-1, respectively. T-226296 can be used for study of obesity and insulin resistance.
For research use only. We do not sell to patients.
- CAS No.: 331758-35-1
- Formula: C26H27FN2O
- Molecular Weight:402.50
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
14 nM
Compound: 1h
|
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting
|
[PMID: 21856163] |
| CHO | IC50 |
24 nM
Compound: 1h
|
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting
|
[PMID: 21856163] |
| CHO | IC50 |
43 nM
Compound: 1h
|
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting
|
[PMID: 21856163] |
| CHO | IC50 |
5.5 nM
Compound: 1, T-226296
|
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay
|
[PMID: 21190859] |
| CHO | IC50 |
5.5 nM
Compound: 7
|
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
Inhibition of Melanin-concentrating hormone 1 receptor expressed in CHO cells
|
[PMID: 15267235] |
| CHO | IC50 |
5.5 nM
Compound: T-226296
|
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
Displacement of [125I]-MCH(4-19) from human MCHR1 expressed in CHO cells
|
[PMID: 21975069] |
| HEK293 | IC50 |
5.5 nM
Compound: I, T-226296
|
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay
|
[PMID: 19773162] |
| IMR-32 | IC50 |
872 nM
Compound: T-226296 (-)
|
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader
|
[PMID: 15341943] |
Chemical Information
-
CAS No. 331758-35-1
-
Molecular Weight 402.50
-
Formula C26H27FN2O
-
SMILES
O=C(C1=CC=C(C2=CC=C(C=C2)F)C=C1)NC3=CC=C(CC(CC4)CN(C)C)C4=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)